title: Bioavailability of Sulforaphane from two broccoli sprout beverages: results of a short-term, cross-over clinical trial in Qidong, China.
abstract: One of several challenges in design of clinical chemoprevention trials is the selection of the dose, formulation, and dose schedule of the intervention agent. Therefore, a cross-over clinical trial was undertaken to compare the bioavailability and tolerability of sulforaphane from two of broccoli sprout-derived beverages: one glucoraphanin-rich (GRR) and the other sulforaphane-rich (SFR). Sulforaphane was generated from glucoraphanin contained in GRR by gut microflora or formed by treatment of GRR with myrosinase from daikon (Raphanus sativus) sprouts to provide SFR. Fifty healthy, eligible participants were requested to refrain from crucifer consumption and randomized into two treatment arms. The study design was as follows: 5-day run-in period, 7-day administration of beverages, 5-day washout period, and 7-day administration of the opposite intervention. Isotope dilution mass spectrometry was used to measure levels of glucoraphanin, sulforaphane, and sulforaphane thiol conjugates in urine samples collected daily throughout the study. Bioavailability, as measured by urinary excretion of sulforaphane and its metabolites (in approximately 12-hour collections after dosing), was substantially greater with the SFR (mean = 70%) than with GRR (mean = 5%) beverages. Interindividual variability in excretion was considerably lower with SFR than with GRR beverage. Elimination rates were considerably slower with GRR, allowing for achievement of steady-state dosing as opposed to bolus dosing with SFR. Optimal dosing formulations in future studies should consider blends of sulforaphane and glucoraphanin as SFR and GRR mixtures to achieve peak concentrations for activation of some targets and prolonged inhibition of others implicated in the protective actions of sulforaphane. Cancer Prev Res; 4(3); 384-95. ©2011 AACR.
authors.affiliation: Department of Environmental Health Sciences, Bloomberg School of Public Health, Johns Hopkins University, Baltimore, MD, USA.
authors.forename: Patricia A
authors.initials: PA
authors.lastname: Egner
authors.forename: Jian Guo
authors.initials: JG
authors.lastname: Chen
authors.forename: Jin Bing
authors.initials: JB
authors.lastname: Wang
authors.forename: Yan
authors.initials: Y
authors.lastname: Wu
authors.forename: Yan
authors.initials: Y
authors.lastname: Sun
authors.forename: Jian Hua
authors.initials: JH
authors.lastname: Lu
authors.forename: Jian
authors.initials: J
authors.lastname: Zhu
authors.forename: Yong Hui
authors.initials: YH
authors.lastname: Zhang
authors.forename: Yong Sheng
authors.initials: YS
authors.lastname: Chen
authors.forename: Marlin D
authors.initials: MD
authors.lastname: Friesen
authors.forename: Lisa P
authors.initials: LP
authors.lastname: Jacobson
authors.forename: Alvaro
authors.initials: A
authors.lastname: Muñoz
authors.forename: Derek
authors.initials: D
authors.lastname: Ng
authors.forename: Geng Sun
authors.initials: GS
authors.lastname: Qian
authors.forename: Yuan Rong
authors.initials: YR
authors.lastname: Zhu
authors.forename: Tao Yang
authors.initials: TY
authors.lastname: Chen
authors.forename: Nigel P
authors.initials: NP
authors.lastname: Botting
authors.forename: Qingzhi
authors.initials: Q
authors.lastname: Zhang
authors.forename: Jed W
authors.initials: JW
authors.lastname: Fahey
authors.forename: Paul
authors.initials: P
authors.lastname: Talalay
authors.forename: John D
authors.initials: JD
authors.lastname: Groopman
authors.forename: Thomas W
authors.initials: TW
authors.lastname: Kensler
mesh_terms: D000328:Adult; D000368:Aged; D016588:Anticarcinogenic Agents / Q000493:pharmacokinetics / Q000652:urine; D001628:Beverages; D001682:Biological Availability; D001937:Brassica; D002681:China; D018592:Cross-Over Studies; D005260:Female; D005838:Genotype; D005961:Glucosinolates / Q000378:metabolism; D006026:Glycoside Hydrolases / Q000737:chemistry; D006801:Humans; D007096:Imidoesters / Q000378:metabolism; D017879:Isothiocyanates; D008297:Male; D008875:Middle Aged; D010091:Oximes; D031224:Raphanus / Q000378:metabolism*; D015203:Reproducibility of Results; D015398:Signal Transduction; D013438:Sulfhydryl Compounds / Q000737:chemistry; D013454:Sulfoxides; D013861:Thiocyanates / Q000493:pharmacokinetics* / Q000652:urine*; D016896:Treatment Outcome
chemical_list: D016588:Anticarcinogenic Agents; D005961:Glucosinolates; D007096:Imidoesters; D017879:Isothiocyanates; D010091:Oximes; D013438:Sulfhydryl Compounds; D013454:Sulfoxides; D013861:Thiocyanates; D006026:Glycoside Hydrolases; C022739:thioglucosidase; C016766:sulforaphane; C119494:glucoraphanin